Mechanism of action

The action of cabergoline stimulates the dopamine receptors in the pituitary gland, reducing the secretion of prolactin from the lactotroph cells. This reduction in prolactin secretion is responsible for the drug’s therapeutic effects in hyperprolactinemia and other conditions associated with elevated prolactin levels

In Parkinson’s disease, cabergoline works by enhancing the effect of dopamine in the brain and improving the symptoms of the disease, such as tremors, rigidity, and bradykinesia

Spectrum

It has a broad spectrum of activity, which is why it treats various conditions. In addition to hyperprolactinemia and Parkinson’s disease, cabergoline has also been used to treat infertility, uterine fibroids, and obsessive-compulsive disorder

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined:

>10%

headache (26%)

nausea (27%)

dizziness (15%)

1-10%

fatigue (7%)

somnolence (5%)

depression (3%)

nervousness (2%)

breast pain (1%)

hot flashes (1%)

constipation (10%)

asthenia (9%)

abdominal pain (5%)

postural hypotension (4%)

dyspepsia (2%)

abnormal vision (1%)

dysmenorrhea (1%)

paresthesia (1%)

<1%

fibrosis

valvulopathy

pleural effusion

aggression

gastric ulcer

psychosis

Post-marketing reports

increased libido and pathological gambling

hypersexuality

 

 

Contraindications

• Hypersensitivity to ergot derivatives is a contraindication for using certain medications derived from ergot, as it can cause an allergic reaction
• The severe hepatic disease can also contraindicate the use of certain medications, as the liver may not be able to metabolize and eliminate the drug from the body properly
• Concurrent use with D2 antagonists refers to medications that block dopamine receptors and can interact with other medications in potentially dangerous ways.
• A history of pulmonary, pericardial, or retroperitoneal fibrotic disorders can make sure medical treatments inadvisable as they can worsen these conditions

Caution

There are several cautions and potential side effects associated with its use:

• Cardiac valvulopathy has been associated with a risk of developing valvular heart disease, particularly in patients who have taken it for prolonged periods
• Nausea and vomiting: It can cause nausea and vomiting, especially during the first few weeks of treatment
• Dizziness: Some patients may experience dizziness or lightheadedness while taking cabergoline
• Mental changes: It has been associated with psychiatric adverse effects such as hallucinations, confusion, and mood changes.
• Pulmonary fibrosis: Long-term use of cabergoline has been associated with an increased risk of developing pulmonary fibrosis, a condition that causes scarring of the lungs
• Liver damage: It can cause liver damage, particularly in patients with liver disease
• Interaction with other medications: It may interact with other medications, including drugs used to treat Parkinson’s, heart disease, and depression

Pregnancy consideration: B

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

cabergoline has a long half-life and is taken orally, usually once or twice a week. After oral administration, it is absorbed rapidly and reaches peak plasma concentrations in about 2-5 hours. cabergoline is highly lipophilic and is widely distributed throughout the body, including the central nervous system. It is primarily metabolized in the liver and excreted in the urine

The main therapeutic effect of cabergoline is its ability to lower elevated prolactin levels in patients with hyperprolactinemia. By decreasing prolactin secretion, cabergoline can alleviate symptoms such as infertility, galactorrhea, and hypogonadism. cabergoline is also used to treat Parkinson’s disease by increasing dopamine levels in the brain, which can improve motor symptoms such as tremors and rigidity

Pharmacodynamics

The pharmacodynamics of cabergoline can be described as follows:

• Binding to dopamine receptors: cabergoline binds to and activates dopamine receptors, leading to an increased release of dopamine. This increased release of dopamine is believed to play a role in the therapeutic effects of cabergoline in treating hyperprolactinemia and Parkinson’s disease
• Decreased prolactin secretion: By binding to the dopamine receptors, cabergoline reduces the secretion of prolactin from the pituitary gland. This is why cabergoline is effective in treating hyperprolactinemia, a condition in which there are elevated levels of prolactin in the blood
• Increased dopamine levels: In patients with Parkinson’s disease, cabergoline increases the levels of dopamine in the brain, which can improve motor symptoms such as tremors and rigidity.
• Receptor selectivity: cabergoline has a high affinity for the dopamine D2 receptor, the primary receptor in regulating prolactin secretion. This high affinity for the D2 receptor makes cabergoline a highly selective and effective medication for treating hyperprolactinemia.
• Long half-life: cabergoline has a long half-life, which allows for once or twice weekly dosing. This can improve patient compliance and convenience compared to other dopamine receptor agonists that need to be taken more frequently

Pharmacokinetics

Absorption

cabergoline is rapidly absorbed after oral administration and reaches peak plasma concentrations in about 2-3 hours. The half-life of cabergoline is approximately 63-69 hours, which allows for once or twice weekly dosing. The peak plasma concentration of cabergoline is typically 30-70 pg/mL following single oral doses of 0.5-1.5 mg

Distribution

cabergoline is highly lipophilic and is widely distributed throughout the body, including the central nervous system. It is bound to 40-42% of plasma proteins

Metabolism

It is extensively hydrolyzed in the liver by a variety of enzymes. The primary metabolites of cabergoline are inactive and do not contribute to its therapeutic effects

Elimination/Excretion

It is excreted primarily in the feces (60%) and, to a lesser extent, in the urine (22%). The half-life of cabergoline is approximately 63-69 hours, which allows for once or twice weekly dosing

Administration

Hyperprolactinemia: For the treatment of hyperprolactinemia, the usual starting dose of cabergoline is 0.5 mg once or twice a week. The dose may be increased as needed, up to 2 mg per week

Parkinson’s disease: For treating Parkinson’s disease, the starting dose of cabergoline is 0.5 mg twice a week. The dose may be increased as needed, up to 5 mg per week

Dosing frequency: cabergoline has a long half-life, which allows for once or twice weekly dosing. The frequency of administration may be adjusted based on the response of the patient and the severity of the condition being treated

Timing of administration: cabergoline should be taken simultaneously daily, with or without food. It is essential to follow the doctor’s dosing schedule and not take more or less of the medication than prescribed

Missed doses: If a dose is missed, it should be taken as soon as possible. If it is almost time for the next dose, the missed dose should be skipped, and the next dose should be taken regularly

Patient information leaflet

Generic Name: cabergoline

Pronounced: [ ca-BER-goe-leen ]

Why do we use cabergoline?

• Hyperprolactinemia: cabergoline is used to treat hyperprolactinemia, a condition in which there is an excess of prolactin in the blood. Prolactin is a hormone that stimulates milk production in the breasts. Cabergoline reduces the secretion of prolactin and can restore regular menstrual periods and fertility in women with hyperprolactinemia
• Parkinson’s disease: cabergoline is also an adjunctive treatment for Parkinson’s disease, a neurodegenerative disorder characterized by tremors, muscle rigidity, and bradykinesia. Cabergoline can help improve symptoms of Parkinson’s disease, including motor fluctuations and dyskinesia
• Prolactin-secreting tumors: cabergoline is used to treat prolactin-secreting tumors, also known as prolactinomas, which are rare tumors of the pituitary gland that cause an excess of prolactin in the blood. Cabergoline can shrink the size of the tumor and reduce the secretion of prolactin
• Fibrotic disorders: cabergoline has been used to treat fibrotic disorders, such as pulmonary fibrosis and retroperitoneal fibrosis, by reducing the levels of prolactin, which has been shown to play a role in the development of these conditions